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  • Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.

Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.

Bioorganic & medicinal chemistry (2010-06-24)
Yong-Hong Liang, Qiu-Qin He, Zhao-Sen Zeng, Zhi-Qian Liu, Xiao-Qing Feng, Fen-Er Chen, Jan Balzarini, Christophe Pannecouque, Erik De Clercq
PMID20570527
ABSTRACT

Nine newly 6-cyano-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC₅₀ of 0.16 and 0.15 μM, and were more activity than that of efavirenz.